1g4k

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(New page: 200px<br /> <applet load="1g4k" size="450" color="white" frame="true" align="right" spinBox="true" caption="1g4k, resolution 2.0&Aring;" /> '''X-ray Structure of a...)
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[[Image:1g4k.gif|left|200px]]<br />
 
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<applet load="1g4k" size="450" color="white" frame="true" align="right" spinBox="true"
 
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caption="1g4k, resolution 2.0&Aring;" />
 
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'''X-ray Structure of a Novel Matrix Metalloproteinase Inhibitor Complexed to Stromelysin'''<br />
 
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==Overview==
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==X-ray Structure of a Novel Matrix Metalloproteinase Inhibitor Complexed to Stromelysin==
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A new class of matrix metalloproteinase (MMP) inhibitors has been, identified by screening a collection of compounds against stromelysin. The, inhibitors, 2,4,6-pyrimidine triones, have proven to be potent inhibitors, of gelatinases A and B. An X-ray crystal structure of one representative, compound bound to the catalytic domain of stromelysin shows that the, compounds bind at the active site and ligand the active-site zinc. The, pyrimidine triones mimic substrates in forming hydrogen bonds to key, residues in the active site, and provide opportunities for placing, appropriately chosen groups into the S1' specificity pocket of MMPS: A, number of compounds have been synthesized and assayed against stromelysin, and the variations in potency are explained in terms of the binding mode, revealed in the X-ray crystal structure.
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<StructureSection load='1g4k' size='340' side='right'caption='[[1g4k]], [[Resolution|resolution]] 2.00&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[1g4k]] is a 3 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1G4K OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=1G4K FirstGlance]. <br>
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</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2&#8491;</td></tr>
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=HQQ:5-METHYL-5-(4-PHENOXY-PHENYL)-PYRIMIDINE-2,4,6-TRIONE'>HQQ</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=1g4k FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1g4k OCA], [https://pdbe.org/1g4k PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=1g4k RCSB], [https://www.ebi.ac.uk/pdbsum/1g4k PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=1g4k ProSAT]</span></td></tr>
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</table>
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== Disease ==
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[https://www.uniprot.org/uniprot/MMP3_HUMAN MMP3_HUMAN] Defects in MMP3 are the cause of susceptibility to coronary heart disease type 6 (CHDS6) [MIM:[https://omim.org/entry/614466 614466]. A multifactorial disease characterized by an imbalance between myocardial functional requirements and the capacity of the coronary vessels to supply sufficient blood flow. Decreased capacity of the coronary vessels is often associated with thickening and loss of elasticity of the coronary arteries. Note=A polymorphism in the MMP3 promoter region is associated with the risk of coronary heart disease and myocardial infarction, due to lower MMP3 proteolytic activity and higher extracellular matrix deposition in atherosclerotic lesions.<ref>PMID:8662692</ref> <ref>PMID:12477941</ref>
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== Function ==
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[https://www.uniprot.org/uniprot/MMP3_HUMAN MMP3_HUMAN] Can degrade fibronectin, laminin, gelatins of type I, III, IV, and V; collagens III, IV, X, and IX, and cartilage proteoglycans. Activates procollagenase.
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== Evolutionary Conservation ==
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[[Image:Consurf_key_small.gif|200px|right]]
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Check<jmol>
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<jmolCheckbox>
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<scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/g4/1g4k_consurf.spt"</scriptWhenChecked>
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<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked>
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<text>to colour the structure by Evolutionary Conservation</text>
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</jmolCheckbox>
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</jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/main_output.php?pdb_ID=1g4k ConSurf].
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<div style="clear:both"></div>
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==Disease==
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==See Also==
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Known diseases associated with this structure: Coronary heart disease, susceptibility to OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=185250 185250]]
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*[[Matrix metalloproteinase 3D structures|Matrix metalloproteinase 3D structures]]
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== References ==
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==About this Structure==
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<references/>
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1G4K is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with ZN, CA, HQQ and GOL as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Stromelysin_1 Stromelysin 1], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.24.17 3.4.24.17] Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=1G4K OCA].
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__TOC__
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</StructureSection>
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==Reference==
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X-ray structure of a novel matrix metalloproteinase inhibitor complexed to stromelysin., Dunten P, Kammlott U, Crowther R, Levin W, Foley LH, Wang P, Palermo R, Protein Sci. 2001 May;10(5):923-6. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=11316871 11316871]
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[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: Single protein]]
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[[Category: Large Structures]]
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[[Category: Stromelysin 1]]
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[[Category: Crowther R]]
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[[Category: Crowther, R.]]
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[[Category: Dunten P]]
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[[Category: Dunten, P.]]
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[[Category: Foley LH]]
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[[Category: Foley, L.H.]]
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[[Category: Kammlott U]]
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[[Category: Kammlott, U.]]
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[[Category: Levin W]]
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[[Category: Levin, W.]]
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[[Category: Palermo R]]
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[[Category: Palermo, R.]]
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[[Category: Wang P]]
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[[Category: Wang, P.]]
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[[Category: CA]]
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[[Category: GOL]]
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[[Category: HQQ]]
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[[Category: ZN]]
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[[Category: mmp]]
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[[Category: stomelysin]]
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[[Category: zinc ligand]]
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''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Nov 12 17:00:38 2007''
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Current revision

X-ray Structure of a Novel Matrix Metalloproteinase Inhibitor Complexed to Stromelysin

PDB ID 1g4k

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